Binding of dihydropyridine calcium antagonists to membranes from human skeletal muscle.

نویسندگان

  • O Krizanová
  • J Orlický
  • J Zachar
چکیده

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Calcium binding to extracellular sites of skeletal muscle calcium channels regulates dihydropyridine binding.

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A QUANTUM CHEMICAL STUDY OF STRUCTURE -ACTIVITY RELATIONSHIPS OF DIHYDROPYRIDINE CALCIUM ANTAGONISTS

Quantum chemical (MNDo)caleulations have beenused toelucidate the molecular properties and structure - activity relationships of dihydropyridine (DHP) type calcium antagonists. There is a good corielation between the net atomic charges on various atoms of the 4 - phenyl ring of dihydropyridines and pharmacological activity. .Also, activity decreases with increasing free rotation of the phen...

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Dihydropyridine and phenylalkylamine receptors associated with cardiac and skeletal muscle calcium channels are structurally different.

We have purified putative L-type Ca2+ channels from chick heart by virtue of their associated high affinity receptors for the Ca2+ channel effectors, dihydropyridines (DHPs), and phenylalkylamines (PAAs). A peptide of 185,000-190,000 daltons was found to comigrate with the peak of DHP binding activity during purification through two successive cycles of lectin affinity chromatography and sucros...

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Reduced calcium sensitivity of dihydropyridine binding to calcium channels in spontaneously hypertensive rats.

To explore the role of calcium channels in hypertension, dihydropyridine ([3H]PN200-110) binding to heart, brain, and skeletal muscle microsomes of 4-, 8- and 15-week-old spontaneously hypertensive rats (SHR) and Wistar-Kyoto (WKY) rats was measured. At a constant Ca2+ ion concentration (pCa 3.0), maximal binding (Bmax) of dihydropyridine binding to heart and brain microsomes was significantly ...

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عنوان ژورنال:
  • General physiology and biophysics

دوره 7 3  شماره 

صفحات  -

تاریخ انتشار 1988